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Miembros

Juan José Vaquero

Juan José Vaquero López
Group coordinator
Full Professor

Publons: E-8310-2012

• Emeritus Professor, Universidad de Alcalá (2023)
• Full Professor Organic Chemistry, Universidad de Alcalá (1998)
• Associate Professor, Universidad de Alcalá (1986)
• Interim Associate Professor, Universidad de Alcalá (1982-1986)
• Postdoctoral researcher, Prof. Charles Rees group, Imperial College London (1985-1986)
• FPI grant (Ministerio de Educación y Ciencia) Universidad de Alcalá (1978-1981)
• Graduated at the Universidad Complutense de Madrid (1976)

Coordinator of Biological Chemistry group, created in 1995, with chemists, pharmacists and molecular biologists developing projects in the field of Medical, Heterocyclic and Bioorganics Chemistry. During this time, the research has been carried out in different lines, among which the following stand out due to their duration and results: Chemistry and applications of heteroaromatic cations in cell staining and bioimaging, synthesis of heterocycles and bioactive alkaloids, design and synthesis of bioactive compounds against targets involved in renal and chemical disease, and applications of azaborines.
In this period, we have participated in 27 R&D&I projects financed in competitive calls from public administrations (Plan Nacional, Comunidad Autónoma de Madrid, Instituto de Salud Carlos III (RETICS), INNPACTO), having acted as PI in 18 of these projects. It has participated in 59 non-competitive R&D&I contracts, agreements or projects financed with administrations and public entities and private companies, acting as PI in 43 of these contracts/projects. The results obtained are summarized in 175 publications in JCR-indexed journals, 29 patents (2 international, 4 PCT), 220 contributions to national and international conferences and the supervision of 24 Doctoral Theses, 10 Theses and 8 Master’s Theses.
He has participated as co-author in three book chapters published by international publishers (Jai Press LTD, UK and Wiley-VCH Verlag) and co-editor together with Prof. Jose Barluenga and Prof. Julio Alvarez-Builla of the 4 volumes of Modern Heterocyclic Chemistry. pp. 1 – 2445 (Germany), WILEY-VCH Verlag GmbH & Co. KGaA (2011).
He has held the academic positions of Dean of the Faculty of Chemistry of the Universidad de Alcalá (2000-2006), Vice-Dean of the Faculty of Science (1987-2000), Scientific Director of the Centre for Applied Chemistry and Biotechnology of the University of Alcalá (2009-2011), 2012-2014, 2015-2017, 2018…), Coordinator by the Universidad de Alcalá of the Inter-University Master in Drug Discovery (2013…) and Trustee appointed by the Universidad de Alcalá in the Board of Trustees of the IMDEA-AGUA Institute of the Comunidad de Madrid (2009…). He has also chaired the Madrid Territorial Section of the Spanish Royal Society of Chemistry for the period 2006-2011.

Publications in the group

Identification and study of new NF-κB-inducing kinase ligands derived from the imidazolone scaffold.
Francisco Maqueda-Zelaya, Lara Valiño-Rivas, Ana Milián, Sara Gutiérrez, José Luis Aceña, Javier Garcia-Marin, Mª Dolores Sánchez-Niño, Juan J Vaquero, Alberto Ortiz
Arch Pharm (Weinheim). 2025 Jan;358(1):e2400614. doi: 10.1002/ardp.202400614. Epub 2024 Nov 27.
Synthesis of Seven- and Eight-Membered Rings by a Brønsted Acid Catalyzed Cationic Carbocyclization of Biphenyl Embedded Enynes.
Jaime Tostado, Ana Milián, Juan J Vaquero, Manuel A Fernández-Rodríguez
Org Lett. 2024 Apr 26;26(16):3343-3348. doi: 10.1021/acs.orglett.4c00647. Epub 2024 Apr 11.
Plaza 3055
Ana Milián, Lucía Sánchez-Jiménez, Jaime Tostado, Juan J. Vaquero, Manuel A. Fernández-Rodríguez, Patricia García-García
Advanced Synthesis & Catalysis. 2024; 366(2):232 -240.
1,2,3-Benzotriazine Synthesis by Heterocyclization of p-Tosylmethyl Isocyanide Derivatives.
Francisco Maqueda-Zelaya, José Luis Aceña, Estíbaliz Merino, Juan J. Vaquero, David Sucunza
J. Org. Chem. 2023, 88, 14131
One-Pot (3 + 2) Cycloaddition-Isomerization-Oxidation of 2,2,2-Trifluorodiazoethane and Styryl Derivatives.
Julia Altarejos, Estíbaliz Merino, David Sucunza, Juan J Vaquero, Javier Carreras
J Org Chem. 2023, 88, 11258
β-Functionalization of 4 a-aza-8 a-boranaphthalene via Iridium-catalyzed C−H Borylation.
Isabel Valencia, David Sucunza, Francisco Mendicuti, Patricia García-García, Juan J. Vaquero
Adv. Synth. Catal. 2023, 365, 2545
Visible-Light-Mediated Regioselective Chlorosulfonylation of Acrylamides.
Mercedes Zurro, Sergio Torres-Oya, Guillermo G. Otárola, Juan José Vaquero, Estíbaliz Merino
Synthesis 2023, 55, 1783
Gold-catalyzed endo-selective cyclization of alkynylcyclobutanecarboxamides: synthesis of cyclobutane-fused dihydropyridones.
M Soledad Garre, Guillermo G Otárola, Estíbaliz Merino, David Sucunza, Enrique Aguilar, M Teresa Quirós, Juan J Vaquero, Patricia García-García
Org Biomol Chem. 2023, 21, 2705
Synthesis of Five-Membered Organoborate Heterocycles via a Metal-Free Carboboration and Their Use in Cross-Coupling Reactions.
Isabel Valencia, David Sucunza, Patricia García-García, Adrián Pérez-Redondo, Juan J. Vaquero
Synthesis 2023, 55, 1260
Synthesis of Phenanthrene-Based Polycycles by Gold(I)-Catalyzed Cyclization of Biphenyl-Embedded Trienynes.
Ana Milián, Patricia García-García, Juan J. Vaquero, Roberto Sanz, Manuel A. Fernández-Rodríguez
Adv. Synth. Catal. 2022, 364, 3960
Highly efficient unbridged D-A+(D) chromophores based on the quinolizinium cation for nonlinear optical (NLO) applications.
Esmeralda Sánchez-Pavón, Javier Recio, Marco Antonio Ramirez, Belen Batanero, Koen Clays, Francisco Mendicuti, Gema Marcelo, Thais Carmona, Obis Castaño, Silvia Angelova, Jose L. Andres, Juan J. Vaquero, Ana M. Cuadro
Dyes Pigm. 2022, 205, 110323.
Synthesis of BN-Polyarenes by a Mild Borylative Cyclization Cascade.
Ester Sans-Panadés, Juan J Vaquero, Manuel A Fernández-Rodríguez, Patricia García-García
Org Lett. 2022, 24, 5860
Steviol glycosides as an alternative osmotic agent for peritoneal dialysis fluid.
Valeria Kopytina, Lucía Pascual-Antón, Nora Toggweiler, Eva-María Arriero-País, Lisa Strahl, Patricia Albar-Vizcaíno, David Sucunza, Juan J Vaquero, Sonja Steppan, Dorothea Piecha, Manuel López-Cabrera, Guadalupe-Tirma González-Mateo
Front Pharmacol. 2022, 13, 868374
Insight into the mechanism of molecular recognition between human Integrin-Linked Kinase and Cpd22 and its implication at atomic level.
Javier García-Marín, Diego Rodríguez-Puyol, Juan J Vaquero
J Comput Aided Mol Des. 2022 Aug;36(8):575-589. doi: 10.1007/s10822-022-00466-1.
Metal-Free Temperature-Controlled Regiodivergent Borylative Cyclizations of Enynes: BCl(3) -Promoted Skeletal Rearrangement.
Ana Milián, Manuel A Fernández-Rodríguez, Estíbaliz Merino, Juan J Vaquero, Patricia García-García
Angew Chem Int Ed Engl. 2022, e202205651
Pyridazino-pyrrolo-quinoxalinium salts as highly potent and selective leishmanicidal agents targeting trypanothione reductase.
Héctor de Lucio, Javier García-Marín, Patricia Sánchez-Alonso, Juan Carlos García-Soriano, Miguel Ángel Toro, Juan J Vaquero, Federico Gago, Ramón Alajarín, Antonio Jiménez-Ruiz
Eur J Med Chem. 2022, 227, 113915
1,10a-Dihydro-1-aza-10a-boraphenanthrene and 6a,7-Dihydro-7-aza-6a-boratetraphene: Two New Fluorescent BN-PAHs.
Isabel Valencia, Patricia García-García, David Sucunza, Francisco Mendicuti, Juan J Vaquero
J Org Chem. 2021 Nov 22. doi: 10.1021/acs.joc.1c01095.
Two-photon activated precision molecular photosensitizer targeting mitochondria.
Inês F. A. Mariz, Sandra N. Pinto, Ana M. Santiago, José M. G. Martinho, Javier Recio, Juan J. Vaquero, Ana M. Cuadro, Ermelinda Maçôas
2021; 4(1):142.
A Computer-Driven Scaffold-Hopping Approach Generating New PTP1B Inhibitors from the Pyrrolo%1,2-a%quinoxaline Core.
Javier García-Marín, Mercedes Griera, Ramón Alajarín, Manuel Rodríguez-Puyol, Diego Rodríguez-Puyol, Juan J Vaquero
ChemMedChem. 2021 Sep 16;16(18):2895-2906. doi: 10.1002/cmdc.202100338.
Enantioselective Copper-Catalyzed Synthesis of Trifluoromethyl-Cyclopropylboronates.
Julia Altarejos, David Sucunza, Juan J Vaquero, Javier Carreras
Org Lett. 2021 Aug 6;23(15):6174-6178. doi: 10.1021/acs.orglett.1c02420.
Pyrrolo%1,2-a%quinoxal-5-inium salts and 4,5-dihydropyrrolo%1,2-a%quinoxalines: Synthesis, activity and computational docking for protein tyrosine phosphatase 1B.
Patricia Sánchez-Alonso, Mercedes Griera, Javier García-Marín, Manuel Rodríguez-Puyol, Ramón Alajarín, Juan J Vaquero, Diego Rodríguez-Puyol
Bioorg Med Chem. 2021 Jul 3; 44:116295.
Tripeptides as Integrin-Linked Kinase Modulating Agents Based on a Protein-Protein Interaction with α-Parvin.
Javier Garcia-Marin, Mercedes Griera-Merino, Alejandra Matamoros-Recio, Sergio de Frutos, Manuel Rodríguez-Puyol, Ramón Alajarín, Juan J Vaquero, Diego Rodríguez-Puyol
ACS Med Chem Lett. 2021 Jul 15;12(11):1656-1662. doi: 10.1021/acsmedchemlett.1c00183.
Recent developments in the chemistry of BN-aromatic hydrocarbons.
Alberto Abengozar, Patricia Garcia-Garcia, Manuel A. Fernández-Rodríguez, David Sucunza, Juan J Vaquero
Adv. Heterocycl. Chem. 2021 Mar 28; :197-259.
A new family of fluorescent pyridazinobenzimidazolium cations with DNA binding properties.
Pedro Bosch, Gema Marcelo, Alejandra Matamoros-Recio, David Sucunza, Francisco Mendicuti, Alberto Domingo, Juan J Vaquero
Dyes and Pigments. 2021 Aug 1; :109443.
Selective Synthesis of Phenanthrenes and Dihydrophenanthrenes via Gold-Catalyzed Cycloisomerization of Biphenyl Embedded Trienynes.
Ana Milián, Patricia García-García, Adrián Pérez-Redondo, Roberto Sanz, Juan J Vaquero, Manuel A Fernández-Rodríguez
Org Lett. 2020, 22, 8464
Gold-Catalyzed Synthetic Strategies towards Four-Carbon Ring Systems.
Guillermo G Otarola, Juan J Vaquero, Estíbaliz Merino, Manuel A Fernández-Rodríguez
Catalysts 2020, 22, 1178
Pyrrolo%@5B1,2-a%@5Dquinoxalines: Insulin Mimetics that Exhibit Potent and Selective Inhibition against Protein Tyrosine Phosphatase 1B.
Javier García-Marín, Mercedes Griera, Patricia Sánchez-Alonso, Bruno Di Geronimo, Francisco Mendicuti, Manuel Rodríguez-Puyol, Ramón Alajarín, Beatriz de Pascual-Teresa, Juan J Vaquero, Diego Rodríguez-Puyol
ChemMedChem 2020, 15, 1788
The pHLIP system as a vehicle for microRNAs in the kidney.
Verónica Miguel, Carlos Rey, José Luis Aceña, Francisco Maqueda, Carlos Fernández-Hernando, Diego Rodríguez-Puyol, Juan J Vaquero, Santiago Lamas
Nefrologia. 2020, 40, 491
Practical Solvent-Free Microwave-Assisted Hydroboration of Alkynes.
Julia Altarejos, David Sucunza, Juan J Vaquero, Javier Carreras
Eur. J. Org. Chem. 2020, 3024
Expanding the BN-embedded PAH family: 4a-aza-12a-borachrysene.
Alberto Abengozar, Isabel Valencia, Guillermo G Otarola, David Sucunza, Patricia Garcia-Garcia, Adrian Perez-Redondo, Francisco Mendicuti, Juan J Vaquero
Chem Commun 2020, 56, 3669
Synthesis and Photophysical Behavior of a Highly Fluorescent Family of Unsymmetrical Organoboron Complexes Containing 5-(Pyridin-2-ylmethylene)imidazolidine-2,4-dione Moieties.
M Soledad Garre, Raul Losantos, Sara Gutierrez, David Sucunza, Patricia Garcia-Garcia, Diego Sampedro, Juan J Vaquero
J Org Chem. 2020, 85, 441
A New Member of the BN-Phenanthrene Family: Understanding the Role of the B-N Bond Position.
Alberto Abengozar, David Sucunza, Patricia Garcia-Garcia, Diego Sampedro, Adrian Perez-Redondo, Juan J Vaquero
J Org Chem. 2019, 84, 7113
Remarkable effect of alkynyl substituents on the fluorescence properties of a BN-phenanthrene.
Alberto Abengozar, David Sucunza, Patricia Garcia-Garcia, Juan J Vaquero
Beilstein J. Org. Chem. 2019, 15, 1257
NIK as a Druggable Mediator of Tissue Injury.
Lara Valino-Rivas, Juan Jose Vaquero, David Sucunza, Sara Gutierrez, Ana B Sanz, Manuel Fresno, Alberto Ortiz, Maria Dolores Sanchez-Nino
Trends Mol Med. 2019, 25, 341
Synthesis, Functionalization, and Optical Properties of 1,2-Dihydro-1-aza-2-boraphenanthrene and Several Highly Fluorescent Derivatives.
Alberto Abengozar, Patricia Garcia-Garcia, David Sucunza, Diego Sampedro, Adrian Perez-Redondo, Juan J Vaquero
Org Lett. 2019, 21, 2550
Regiodivergent Electrophilic Cyclizations of Alkynylcyclobutanes for the Synthesis of Cyclobutane-Fused O-Heterocycles.
M Soledad Garre, David Sucunza, Enrique Aguilar, Patricia Garcia-Garcia, Juan J Vaquero
J. Org. Chem. 2019, 84, 9, 5712
MAP3K kinases and kidney injury.
Leticia Cuarental, David Sucunza, Lara Valino-Rivas, Beatriz Fernandez-Fernandez, Ana Belen Sanz, Alberto Ortiz, Juan Jose Vaquero, Maria Dolores Sanchez-Nino
Nefrologia 2019, 39, 568
Discovery of potent calpain inhibitors based on the azolo-imidazolidenone.
Sara Gutierrez, Maria Moron, Mercedes Griera, David Sucunza, Laura Calleros, Andrea Garcia-Jerez, Claire Coderch, Francisco J Hermoso, Carolina Burgos, Manuel Rodriguez-Puyol, Beatriz de Pascual-Teresa, Maria L Diez-Marques, Antonio Jimenez, Miguel Toro-Londono, Diego Rodriguez-Puyol, Juan J Vaquero
Eur J Med Chem. 2018, 157, 946
C-H Functionalization of BN-Aromatics Promoted by Addition of Organolithium Compounds to the Boron Atom.
Alberto Abengozar, Miguel Angel Fernandez-Gonzalez, David Sucunza, Luis Manuel Frutos, Antonio Salgado, Patricia Garcia-Garcia, Juan J Vaquero
Org Lett. 2018, 20, 4902
gamma-Carboline Synthesis by Heterocyclization of TosMIC Derivatives.
Sara Gutierrez, David Sucunza, Juan J Vaquero
J Org Chem. 2018, 83, 6623
A Tricin Derivative from Deschampsia antarctica Desv. Inhibits Colorectal Carcinoma Growth and Liver Metastasis through the Induction of a Specific Immune Response.
Mariana Malvicini, Ana Gutierrez-Moraga, Marcelo M Rodriguez, Sofia Gomez-Bustillo, Lorena Salazar, Carlos Sunkel, Leonor Nozal, Antonio Salgado, Manuel Hidalgo, Pedro P Lopez-Casas, Jose Luis Novella, Juan Jose Vaquero, Julio Alvarez-Builla, Adda Mora, Manuel Gidekel, Guillermo Mazzolini
Mol Cancer Ther. 2018 May;17(5):966-976. doi: 10.1158/1535-7163.MCT-17-0193. Epub 2018 Feb 26.
Dibenzopyridoimidazocinnolinium cations: a new family of light-up fluorescent DNA probes.
Pedro Bosch, David Sucunza, Francisco Mendicuti, Alberto Domingo, Juan J Vaquero
Org. Chem. Front. 2018, 5, 1916
Synthesis of functionalized helical BN-benzo%c%phenanthrenes.
Alberto Abengozar, Patricia Garcia-Garcia, David Sucunza, Adrian Perez-Redondo, Juan J Vaquero
Chem Commun 2018, 54, 2467
Azonia aromatic heterocycles as a new acceptor unit in D-π-A%@2B vs D-A%@2B nonlinear optical chromophores.
Tatiana Cañeque, Ana M. Cuadro, Raúl Custodio, Julio Alvarez-Builla, Belén Batanero, Pilar Gómez-Sal, Javier Pérez-Moreno, Koen Clays, Obis Castaño, José L. Andrés, Thais Carmona, Francisco Mendicuti, Juan J Vaquero
Dyes Pigm. 2017, 144, 17
Microwave-assisted pyrolysis of Mediterranean forest biomass waste: Bioproduct characterization.
María T. Martín, Ana B. Sanz, Leonor Nozal, Flor Castro, Raúl Alonso, Juan L. Aguirre, Sergio D. González, M. Paz Matía, José L. Novella, Manuel Peinado, Juan J Vaquero
J Anal Appl Pyrolysis 2017, 127, 278
Synthesis, Optical Properties, and Regioselective Functionalization of 4a-Aza-10a-boraphenanthrene.
Alberto Abengozar, Patricia Garcia-Garcia, David Sucunza, Luis Manuel Frutos, Obis Castano, Diego Sampedro, Adrian Perez-Redondo, Juan J Vaquero
Org Lett. 2017, 19, 3458
Imidazopyridinium cations: A new family of azonia aromatic heterocycles with applications as DNA intercalators.
Pedro Bosch, Verónica García, Başak S. Bilen, David Sucunza, Alberto Domingo, Francisco Mendicuti, Juan J Vaquero
Dyes Pigm. 2017, 138, 135
Quinolizinium as a new fluorescent lysosomotropic probe.
Emmanouil Zacharioudakis, Tatiana Cañeque, Raúl Custodio, Sebastian Müller, Ana M. Cuadro, Juan J Vaquero, Raphaël Rodriguez
Biorg. Med. Chem. Lett. 2017, 27, 203
Halogen-containing thiazole orange analogues - new fluorogenic DNA stains.
Aleksey A Vasilev, Meglena I Kandinska, Stanimir S Stoyanov, Stanislava B Yordanova, David Sucunza, Juan J Vaquero, Obis D Castano, Stanislav Baluschev, Silvia E Angelova
Beilstein J. Org. Chem. 2017, 13, 2902
Recent Advances in the Synthesis of Azonia Aromatic Heterocycles.
David Sucunza, Ana M Cuadro, Julio Alvarez-Builla, Juan J Vaquero
J Org Chem. 2016, 81, 10126
Synthesis of 1-Substituted Isoquinolines by Heterocyclization of TosMIC Derivatives: Total Synthesis of Cassiarin A.
Sara Gutierrez, Anna Coppola, David Sucunza, Carolina Burgos, Juan J Vaquero
Org Lett. 2016, 18, 3378
Highly Fluorescent Green Fluorescent Protein Chromophore Analogues Made by Decorating the Imidazolone Ring.
Sara Gutierrez, David Martinez-Lopez, Maria Moron, David Sucunza, Diego Sampedro, Alberto Domingo, Antonio Salgado, Juan J Vaquero
Chem. Eur. J. 2015, 21, 18758
Assembly of New Merocyanine Chromophores with a 1,8-Naphthalimide Core by a New Method for the Synthesis of the Methine Function.
Aleksey A. Vasilev, Stanislav Baluschev, Diana Cheshmedzhieva, Sonia Ilieva, Obis D. Castaño, Juan J Vaquero, Silvia E. Angelova, Katharina Landfester
Aust. J. Chem. 2015, 68, 1399
Nonlinear Emission of Quinolizinium Based Dyes With Application in Fluorescence Lifetime Imaging.
Gema Marcelo, Sandra Pinto, Tatiana Cañeque, Inês F. A. Mariz, Ana M. Cuadro, Juan J Vaquero, José M. G. Martinho, Ermelinda M. S. Maçôas
J. Phys. Chem. A 2015, 119, 11, 2351
Azonia Aromatic Cations by Ring-Closing Metathesis: Synthesis ofAzaquinolizinium Cations.
Alberto Abengozar, Beatriz Abarca, Ana M. Cuadro, David Sucunza, Julio Álvarez‐Builla, Juan J Vaquero
Eur J Org Chem. 2015, 6, 4214
Synthesis and biological evaluation of pyridazino%@5B1′,6′:1,2%@5Dpyrido%@5B3,4-b%@5Dindolinium and pyridazino%@5B1,6-a%@5Dbenzimidazolium salts as anti-inflammatory agents.
Aranzazu Rodríguez-Sanz, Patricia Sánchez-Alonso, Teresa Bellón, Ramón Alajarín, Virginia Martínez-Cabeza, Rafael Selgas, Juan J. Vaquero, Julio Álvarez-Builla
Eur. J. Med. Chem. 2015, 93, 83
Isoquinoline synthesis by heterocyclization of tosylmethyl isocyanide derivatives: total synthesis of mansouramycin B.
Anna Coppola, David Sucunza, Carolina Burgos, Juan J Vaquero
Org Lett. 2015, 17, 78
Targeting DNA with small molecules: a comparative study of a library of azonia aromatic chromophores.
Rosa M Suarez, Pedro Bosch, David Sucunza, Ana M Cuadro, Alberto Domingo, Francisco Mendicuti, Juan J Vaquero
Org Biomol Chem. 2015, 13, 527
Efficient synthesis of an indoloquinolizinium alkaloid selective DNA-binder by ring-closing metathesis.
Beatriz Abarca, Raul Custodio, Ana M Cuadro, David Sucunza, Alberto Domingo, Francisco Mendicuti, Julio Alvarez-Builla, Juan J Vaquero
Org Lett. 2014, 16, 3464
Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold.
Ana I Sanchez, Ricardo Meneses, Jose M Minguez, Araceli Nunez, Rafael R Castillo, Fabiana Filace, Carolina Burgos, Juan J Vaquero, Julio Alvarez-Builla, Alvaro Cortes-Cabrera, Federico Gago, Emma Terricabras, Victor Segarra
Org Biomol Chem. 2014, 12, 4233
Cucurbit%n%urils as a potential fine-tuned instrument for modifying photophysical properties of D–π–A+–π–D “push–pull” chromophores.
Thais Carmona, Tatiana Cañeque, Raul Custodio, Ana M. Cuadro, Juan J Vaquero, Francisco Mendicuti
Dyes Pigm. 2014, 103, 106
Novel charged NLO chromophores based on quinolizinium acceptor units.
Tatiana Cañeque, Ana M. Cuadro, Julio Alvarez-Builla, Julio Alvarez-Builla, Javier Pérez-Moreno, Koen Clays, Obis Castaño, José L. Andrés, Juan J Vaquero
Dyes Pigm. 2014, 101, 116
Remote aryl cyanation via isocyanide-cyanide rearrangement on tosylmethyl isocyanide derivatives.
Anna Coppola, Patricia Sanchez-Alonso, David Sucunza, Carolina Burgos, Ramon Alajarin, Julio Alvarez-Builla, Marta E G Mosquera, Juan J Vaquero
Org Lett. 2013 Jul 5;15(13):3388-91. doi: 10.1021/ol401433x. Epub 2013 Jun 24.
A cascade reaction of azolopyrimidines. Synthesis of unusual indole and azaindole derivatives.
María Morón, Carolina Burgos, Julio Alvarez-Builla, Antonio Salgado, Marta E. G. Mosquera, Juan J Vaquero
Chem. Commun. 2012, 48, 9171
Superior Neuroprotective Efficacy of LAU-0901, a Novel Platelet-Activating Factor Antagonist, in Experimental Stroke.
Ludmila Belayev, Tiffany N. Eady, Larissa Khoutorova, Kristal D. Atkins, Andre Obenaus, Marta Cordoba, Juan J. Vaquero, Julio Alvarez-Builla, Nicolas G. Bazan
Translational Stroke Research 2012, 3, 154
Synthesis of 9,9′-%1,2-Ethanediylbis(oxymethylene)%bis-2-amino-1,9-dihydro-6H-purin-6-one, an Impurity of Acyclovir.
Rosa M. Suárez, Maria Paz Matía, José Luis Novella, Andres Molina, Antonio Cosme, Juan José Vaquero, Julio Alvarez-Builla
Molecules 2012, 17, 8735
New losartan-hydrocaffeic acid hybrids as antihypertensive-antioxidant dual drugs: Ester, amide and amine linkers
Gonzalo García, Isabel Serrano, Patricia Sánchez-Alonso, Manuel Rodríguez-Puyol, Ramón Alajarín, Mercedes Griera, Juan J. Vaquero, Diego Rodríguez-Puyol, Julio Álvarez-Builla, María L. Díez-Marqués
Eur. J. Med. Chem 2012, 50, 90
Radical Intramolecular Arylation of Pyridinium Salts: A Straightforward Entry to 7-Hydroxypyrido%2,1‐a%isoquinolinylium Salts /
Rafael R. Castillo, Carolina Burgos, Juan J. Vaquero, Julio Alvarez-Builla
Eur. J. Org. Chem. 2011, 619
An environmentally benign procedure for the synthesis of substituted 2-thiobenzothiazoles, 2-thiobenzoxazoles, 2-thiobenzimidazoles, and 1,3-oxazolopyridine-2-thiols.
Todor G. Deligeorgiev, Stefka S. Kaloyanova, Nedyalko Y. Lesev, Juan J. Vaquero
Monatsh. Chem. 2011, 142, 895
Synthesis of novel tetracationic asymmetric monomeric monomethine cyanine dyes – highly fluorescent dsDNA probes /
Aleksey Vasilev, Todor Deligeorgiev, Stefka Kaloyanova, Stanimir Stoyanov, Vera Maximova, Juan J Vaquero, Julio Alvarez-Builla
Coloration Technology. 2011, 127, 69
Environmental Risk Assessment of Emerging Pollutants in Water: Approaches Under Horizontal and Vertical EU Legislation /
M. D. Hernando, A. Rodríguez, J. J. Vaquero, A. R. Fernández-Alba, E. García
Critical Reviews in Environmental Science and Technology 2011, 41, 699
Ring-Closing Metathesis Approach to Heteroaromatic Cations: Synthesis of Benzo%a%Dquinolizinium Salts /
Ana Nuñez, Beatriz Abarca, Ana M. Cuadro, Julio Alvarez-Builla, Juan J. Vaquero
Eur. J. Org. Chem. 2011, 1280
Heteroaromatic Cation-Based Chromophores: Synthesis and Nonlinear Optical Properties of Alkynylazinium Salts /
Tatiana Cañeque, Ana M. Cuadro, Julio Alvarez-Builla, Javier Pérez-Moreno, Koen Clays, Gema Marcelo, Francisco Mendicuti, Obis Castaño, José L. Andrés, Juan J. Vaquero
Eur. J. Org. Chem. 2010, 6323
Application of Selective Palladium-Mediated Functionalization of the Pyrido%@5B3′,2′:4,5%@5Dpyrrolo%@5B1,2-c%@5Dpyrimidine Heterocyclic System for the Total Synthesis of Variolin B and Deoxyvariolin B /
Alejandro Baeza, Javier Mendiola, Carolina Burgos, Julio Alvarez-Builla, Juan J. Vaquero
Eur. J. Org. Chem. 2010, 5607
Novel Green Procedure for the Synthesis of 2-Arylbenzothiazoles Under Microwave Irradiation in Peg 200 Or Peg 400 /
Todor G. Deligeorgiev, Stefka Kaloyanova, Aleksey Vasilev, Juan J. Vaquero
Phosphorus, Sulfur, and Silicon and the Related Elements 2010, 185, 2292
Styryl dyes – synthesis and applications during the last 15 years /
Todor Deligeorgiev, Aleksey Vasilev, Stefka Kaloyanova, Juan J Vaquero
Coloration Technology. 2010, 126, 55
An easy and fast ultrasonic selective S-alkylation of hetaryl thiols at room temperature /
Todor Deligeorgiev, Stefka Kaloyanova, Nedyalko Lesev, Juan J. Vaquero
Ultrasonics Sonochemistry 2010, 17, 783
Miembros

Patricia García

Patricia García García

Associate Professor

  • Associate Professor, Universidad de Alcalá (2019–)
  • Ramón y Cajal researcher, Universidad de Alcalá (2014-2019)
  • Juan de la Cierva researcher, Prof. R. Sanz group, Universidad de Burgos (2009-2013)
  • Postdoctoral researcher, Prof. B. List group, Max-Planck-Institut für Kohlenforschung (Alemania) (2007-2009)
  • Ph.D. Universidad de Oviedo (2007)), supervisors Prof. J. Barluenga and Prof. E. Aguilar
  • Graduated at the Universidad de Oviedo (2002)

Doctor from the University of Oviedo, with extensive postdoctoral experience in the field of organic synthesis and catalysis. In 2014 she joined the University of Alcalá as a “Ramón y Cajal” researcher and since 2019 she is associate professor at the same university. Her current interests focus on the synthesis and applications of azaborine, the development of new synthetic methodologies based on electrophilic cyclizations of alkynes, and the preparation and evaluation of molecules of interest in medicinal chemistry. During his scientific career he has participated in more than 20 research projects obtained in competitive calls, being PI in several of them, including 3 of national character. His research work has resulted in more than 50 scientific publications and 5 patents. In addition, he has co-directed three doctoral theses and is currently co-directing another 3.

 

2018, Publicación, Renal

Gutierrez et al. Eur J Med Chem. 2018;157:946-959. Discovery of potent calpain inhibitors based on the azolo-imidazolidenone.

Publications > Gutierrez et al

Eur J Med Chem. 2018, 157, 946 PubMed 30165342

Discovery of potent calpain inhibitors based on the azolo-imidazolidenone.

Sara Gutierrez1, Maria Moron1, Mercedes Griera2, David Sucunza1, Laura Calleros2, Andrea Garcia-Jerez2, Claire Coderch3, Francisco J Hermoso3, Carolina Burgos1, Manuel Rodriguez-Puyol2, Beatriz de Pascual-Teresa3, Maria L Diez-Marques2, Antonio Jimenez2, Miguel Toro-Londono2, Diego Rodriguez-Puyol4, Juan J Vaquero1

1. Departamento de Quimica Organica y Quimica Inorganica, Universidad de Alcala.  2. Departamento de Biologia de Sistemas, Universidad de Alcala, 28871, Alcala de.  3. Departamento de Quimica y Bioquimica, Facultad de Farmacia, Universidad San.  4. Research Unit and Nephrology Section, Hospital Principe de Asturias and.

Keywords: Azolo-imidazolidenone; Blockade of apoptosis; Calpain inhibitors; SAR; Uncompetitive inhibition

Abstract

A series of new azolopyrimidine-peptide hybrids and indolomethylideneimidazolones

2018, AzaBN, Publicación

Abengozar et al. Org Lett. 2018;20(16):4902-4906. C-H Functionalization of BN-Aromatics Promoted by Addition of Organolithium Compounds to the Boron Atom.

Publications > Abengozar et al

Org Lett. 2018, 20, 4902 PubMed 30070487

C-H Functionalization of BN-Aromatics Promoted by Addition of Organolithium Compounds to the Boron Atom.

Alberto Abengozar1, Miguel Angel Fernandez-Gonzalez2, David Sucunza1, Luis Manuel Frutos2, Antonio Salgado3, Patricia Garcia-Garcia1, Juan J Vaquero1

1. Departamento de Quimica Organica y Quimica Inorganica, Instituto de Investigacion Quimica "Andres M. del Rio" (IQAR) , Universidad de Alcala , 28805 Alcala de Henares , Madrid , Spain.  2. Departamento de Quimica Analitica, Quimica Fisica e Ingenieria Quimica, Instituto de Investigacion Quimica "Andres M. del Rio" (IQAR) , Universidad de Alcala , 28805 Alcala de Henares , Madrid , Spain.  3. Centro de Espectroscopia de Resonancia Magnetica Nuclear (CERMN), CAI Quimicas , Universidad de Alcala , 28805 Alcala de Henares , Madrid , Spain.

Abstract

Addition of an organolithium compound to a BN-phenanthrene with embedded B and N atoms is proposed to result in coordination of RLi to the boron atom. This coordination, supported by NMR spectroscopy and DFT calculations, increases the nucleophilicity of the system in the beta position to the N atom and is therefore a useful tool for promoting regioselective C-H functionalization of BN aromatics.

2018, Publicación, TosMIC

Gutierrez et al. J Org Chem. 2018;83(12):6623-6632. gamma-Carboline Synthesis by Heterocyclization of TosMIC Derivatives.

Publications > Gutierrez et al

J Org Chem. 2018, 83, 6623 PubMed 29756452

gamma-Carboline Synthesis by Heterocyclization of TosMIC Derivatives.

Sara Gutierrez, David Sucunza, Juan J Vaquero

Departamento de Quimica Organica y Quimica Inorganica and Instituto de Investigacion Quimica "Andres M. del Rio" (IQAR) , Universidad de Alcala , 28805 - Alcala de Henares , Madrid , Spain.

Abstract

A new method for the synthesis of gamma-carbolines by a heterocyclization that involves alpha-indol-2-ylmethyl TosMIC derivatives and different electrophiles has been developed. This methodology has been successfully applied to the synthesis of several highly substituted gamma-carbolines.

2018, Publicación

Malvicini et al. Mol Cancer Ther. 2018;17(5):966-976. A Tricin Derivative from Deschampsia antarctica Desv. Inhibits Colorectal Carcinoma Growth and Liver Metastasis through the Induction of a Specific Immune Response.

Publications > Malvicini et al

Mol Cancer Ther. 2018 May;17(5):966-976. doi: 10.1158/1535-7163.MCT-17-0193. Epub 2018 Feb 26. PubMed 29483221

A Tricin Derivative from Deschampsia antarctica Desv. Inhibits Colorectal Carcinoma Growth and Liver Metastasis through the Induction of a Specific Immune Response.

Mariana Malvicini1, Ana Gutierrez-Moraga2, Marcelo M Rodriguez3, Sofia Gomez-Bustillo1, Lorena Salazar1, Carlos Sunkel2, Leonor Nozal2, Antonio Salgado4, Manuel Hidalgo4, Pedro P Lopez-Casas5, Jose Luis Novella6, Juan Jose Vaquero4, Julio Alvarez-Builla4, Adda Mora4, Manuel Gidekel7, Guillermo Mazzolini2, a

1. Gene Therapy Laboratory, Instituto de Investigaciones en Medicina Traslacional, Facultad de Ciencias Biomedicas, CONICET- Universidad Austral, Buenos Aires, Argentina.  2. Universidad Autonoma de Chile, Providencia, Chile.  3. Universidad de La Frontera, Temuco, Chile.  4. Departamento de Quimica Organica, Universidad de Alcala, Madrid, Spain.  5. Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.  6. Gastrointestinal Cancer Clinical Research Unit, CNIO - Spanish National Cancer Research Center, Madrid, Spain.  7. Creative BioScience, Huechuraba, Santiago, Chile.

a. gmazzoli@cas.austral.edu.ar, mgidekel@creativebio-science.com

Abstract

In colorectal carcinoma patients, distant metastatic disease is present at initial diagnosis in nearly 25% of them. The majority of patients with metastatic colorectal carcinoma have incurable disease; therefore, new therapies are needed. Agents derived from medicinal plants have already demonstrated therapeutic activities in human cancer cells. Antartina is an antitumor agent isolated from Deschampsia antarctica Desv. This study aimed to evaluate the antitumor properties of Antartina in colorectal carcinoma models. We used human and murine colorectal carcinoma cell lines for investigating proliferation, apoptosis, and cell-cycle effects of Antartina therapy in vitro Avatar and immunocompetent colorectal carcinoma animal models were applied for evaluating the effects of Antartina in vivo Immune response against colorectal carcinoma model was investigated using CTL assay, analyzing dendritic cell activation and intratumor T-cell subpopulation, and by tumor rechallenge experiments. Antartina inhibits in vitro human colorectal carcinoma cell proliferation; however, in vivo experiments in Avatar colorectal carcinoma model Antartina display a limited antitumor effect. In an immunocompetent colorectal carcinoma mice model, Antartina potently inhibited tumor growth and liver metastases, leading to complete tumor regressions in >30% of mice and increased animal survival. In addition, Antartina induced a potent specific cytotoxic T-cell response against colorectal carcinoma and a long-lasting antitumor immunity. Interestingly, Antartina increased tumor immunogenicity and stimulated dendritic cell activation. No toxic effects were observed at the doses employed. Our findings showed that Antartina has the ability to induce antitumor immunity against colorectal carcinoma and can be used to develop new tools for the treatment of colorectal carcinoma. Mol Cancer Ther; 17(5); 966-76. (c)2018 AACR.

2018, BioImag, Publicación

Bosch et al. Org. Chem. Front.. 2018;5(12):1916-1927. Dibenzopyridoimidazocinnolinium cations: a new family of light-up fluorescent DNA probes.

Publications > Bosch et al

Org. Chem. Front. 2018, 5, 1916

Dibenzopyridoimidazocinnolinium cations: a new family of light-up fluorescent DNA probes.

Pedro Bosch1, David Sucunza1, Francisco Mendicuti2, Alberto Domingo3, Juan J Vaquero1

1. Departamento de Quimica Organica y Quimica Inorganica, Instituto de Investigacion Quimica "Andres M. del Rio" (IQAR) , Universidad de Alcala , 28805 Alcala de Henares , Spain.  2. Departamento de Química Analítica, Química Física e Ingeniería Química, Universidad de Alcalá, Spain.  3. Departamento de Biología de Sistemas, Universidad de Alcalá, Spain.

Abstract

Steady-state and time-resolved fluorescence, circular dichroism and molecular modelling techniques have been applied to a new family of weakly fluorescent dibenzopyridoimidazocinnolinium derivatives whose fluorescence intensity increases significantly (larger than × 3.5) upon DNA addition. The synthesis of these azonia cations, which bind to DNA by intercalation, was carried out using a Westphal condensation and a Suzuki cross coupling reaction as key steps. A live-cell staining analysis by confocal microscopy imaging was also performed and showed the capacity of these new compounds for active uptake and accumulation by living cells, with complex patterns of intracellular distribution observed.

2018, AzaBN, Publicación

Abengozar et al. Chem Commun (Camb). 2018;54(20):2467-2470. Synthesis of functionalized helical BN-benzo[c]phenanthrenes.

Publications > Abengozar et al

Chem Commun 2018, 54, 2467 PubMed 29319090

Synthesis of functionalized helical BN-benzo[c]phenanthrenes.

Alberto Abengozara, Patricia Garcia-Garcia, David Sucunza, Adrian Perez-Redondo, Juan J Vaquero

Departamento de Quimica Organica y Quimica Inorganica, Instituto de Investigacion Quimica "Andres M. del Rio" (IQAR), Universidad de Alcala, 28805-Alcala de Henares, Madrid, Spain.

a. patricia.garciagarci@uah.es, juanjose.vaquero@uah.es

Abstract

A novel parent BN-benzo[c]phenanthrene, with helical chirality and remarkable structural features, has been easily obtained in three steps with a global yield of 55%. Moreover, Cl-substituted derivatives have been prepared and these have served as useful starting materials for the development of palladium-catalyzed cross-coupling reactions.